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Rational Modification of the Biological Profile of GPCR Ligands through Combination with Other Biologically Active Moieties
Author(s) -
Huang Guozheng,
Nimczick Martin,
Decker Michael
Publication year - 2015
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201500079
Subject(s) - g protein coupled receptor , chemistry , allosteric regulation , biological activity , computational biology , drug discovery , combinatorial chemistry , stereochemistry , receptor , biochemistry , biology , in vitro
In recent years, G protein‐coupled receptor (GPCR) ligands have not only been modified by conducting structure–activity relationship studies of leads and known ligands, but several new approaches have emerged in which GPCR ligands were connected or merged with other biologically active molecules. Identical or related ligands were combined to bivalent ones. Orthosteric ligands were combined with allosteric ligands, sometimes leading to dualsteric ones, and also chemical structures were merged to dual‐acting or multifunctional compounds. In this article, we want to present some representative examples for these approaches at different GPCRs, showing the versatility of this approach, with a focus on our own work and references to related articles and reviews.